Ring Chalcogen And Ring Nitrogen Are In The 1,5-positions Of The Seven-membered Hetero Ring Patents (Class 514/211.06)
  • Patent number: 9914735
    Abstract: The invention relates to new substituted heteroaryls of formula (1), wherein A is selected from the group consisting of N and CH, D is CH, E is selected from the group consisting of C and N, T is C, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: March 13, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Dahmann, Matthias Hoffmann, Jasna Klicic, David James Lamb, Clive McCarthy, Spencer Charles R. Napier, Karen Parrish, John Scott, Jennifer L. Swantek Fitzgerald, Edward Walker
  • Patent number: 9458135
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R9, R10, R11 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: October 4, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Alexander V. Mayweg, Xuefei Tan
  • Patent number: 9051321
    Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: August 20, 2014
    Date of Patent: June 9, 2015
    Assignee: FAB PHARMA S.A.S.
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
  • Publication number: 20150038489
    Abstract: Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blocker
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Sridharan Rajamani, Dewan Zeng
  • Publication number: 20150038488
    Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
    Type: Application
    Filed: July 31, 2014
    Publication date: February 5, 2015
    Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
  • Patent number: 8895545
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: November 25, 2014
    Assignee: Debiopharm International SA
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20140302988
    Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 9, 2014
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140031334
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: September 20, 2013
    Publication date: January 30, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Hideaki KURODA, Nobuaki ITO, Kunio OSHIMA, Jun MATSUBARA, Tae FUKUSHIMA, Satoshi SHIMIZU, Kazumi KONDO, Motohiro ITOTANI
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20130237523
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 12, 2013
    Applicant: AFFINIUM PHARMACEUTICALS, INC.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Publication number: 20130171069
    Abstract: In one or a plurality of embodiments, there is provided a target molecule of amylospheroid, which is expressed in mature neurons and to which the amylospheroid binds to induce death of cells. Further, in one or a plurality of embodiments, there is provided a method and a substance for inhibiting death of mature neurons induced by the amylospheroid. In one aspect, the present disclosure relates to a use of Na+/K+-ATPase ?3 as a binding target molecule of amylospheroid. In another aspect, the present disclosure relates to a method for suppressing death of mature neurons induced by the amylospheroid, including inhibiting protein-protein interaction between the amylospheroid and the Na+/K+-ATPase ?3, and the like.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: TAO HEALTH LIFE PHARMA CO., LTD.
    Inventor: Tao Health Life Pharma Co., Ltd.
  • Publication number: 20120328599
    Abstract: The present invention provides moieties that bind to the asymmetric contact interface of a receptor tyrosine kinase (RTK), wherein the moieties inhibit ligand induced trans autophosphorylation of the RTK. The present invention also provides methods of treating or preventing an RTK-associated disease and methods for identifying moieties that bind to an asymmetric contact interface of an RTK.
    Type: Application
    Filed: January 13, 2011
    Publication date: December 27, 2012
    Applicant: YALE UNIVERSITY
    Inventors: Jae Hyun Bae, Irit Lax, Joseph Schlessinger
  • Patent number: 8318720
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: July 19, 2007
    Date of Patent: November 27, 2012
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Patent number: 8168803
    Abstract: Disclosed are methods of treating cancer, inflammatory conditions, and/or infectious disease in an animal comprising: administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: May 1, 2012
    Assignee: Nereus Pharmaceuticals, Inc.
    Inventors: Michael Palladino, Saskia Theodora Cornelia Neuteboom
  • Publication number: 20120028920
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: October 11, 2011
    Publication date: February 2, 2012
    Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
  • Patent number: 7994161
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 9, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Alain Commerçon
  • Patent number: 7994160
    Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: August 9, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
  • Patent number: 7977326
    Abstract: The invention provides a composition and method for treatment of a subject suffering from liver disease comprising the oral administration of a slow release formulation of calcium channel blocker such as diltiazem and thiamine which is also an antioxidant which is relatively hydrophilic when compared with the calcium channel blocker.
    Type: Grant
    Filed: April 21, 2005
    Date of Patent: July 12, 2011
    Inventor: Howard J Smith
  • Patent number: 7960373
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: June 14, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Frederico Nardi, Alain Commerçon
  • Publication number: 20110123612
    Abstract: The present invention provides a pharmaceutical formulation comprising an immediate-release compartment containing an angiotensin-2 receptor blocker (ARB) as a pharmacologically active ingredient and an extended-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. Since the disclosed formulation enables the release of the two ingredients at a different time, it reduces side effects and increases the effects of the drug more than the case of separately administering the ingredients each at the same time. In addition, the formulation maximizes the effects of drug at the time of day when the complication risk of cardiovascular system diseases is highest.
    Type: Application
    Filed: April 3, 2009
    Publication date: May 26, 2011
    Inventors: Sung Wuk Kim, Sung Soo Jun, Ah Ram Lee, Sang Ouk Sun, Jin Won Choi, Young Gwan Jo, Ja Seong Koo
  • Publication number: 20110118232
    Abstract: The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C?W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N—Rk or a group CRmRn; D represents C?O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N—Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2—CH2 or CH2—CH2—CH2; M represents CH or N; Y represents CH2, CH2—CH2 or CH2—CH2—CH2 or M-X, together, represent CH?C or CH2—CH?C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf,
    Type: Application
    Filed: July 23, 2010
    Publication date: May 19, 2011
    Applicant: Abbott GmbH & Co. KG
    Inventors: Hervè Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
  • Publication number: 20110112067
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Application
    Filed: November 3, 2010
    Publication date: May 12, 2011
    Applicant: Universitat des Saarlandes
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20110086842
    Abstract: The present invention encompasses compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Application
    Filed: December 20, 2010
    Publication date: April 14, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heinz STADTMUELLER, Harald ENGELHARDT, Martin STEEGMAIER, Anke BAUM, Ulrich GUERTLER, Andreas SCHOOP, Jens Juergen QUANT, Flavio SOLCA, Rudolf HAUPTMANN, Ulrich REISER, Stephan Karl ZAHN, Lars HERFURTH
  • Publication number: 20110053910
    Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.
    Type: Application
    Filed: July 3, 2006
    Publication date: March 3, 2011
    Inventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
  • Patent number: 7842686
    Abstract: The present invention relates to CGRP receptor antagonists, pharmaceutical compositions thereof, and methods therewith for treating CGRP receptor-mediated diseases and conditions.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: November 30, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Don Anderson, Andreas P. Termin, Pramod Joshi, Sara S. Hadida Ruah, Daniele Bergeron, Sanghee Yoo, Jingrong Cao
  • Patent number: 7786105
    Abstract: The invention relates to pyrimidine compounds of general formula (I), and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: August 31, 2010
    Assignee: Abbott GmbH & Co. KG
    Inventors: Herve Geneste, Andreas Haupt, Wilfried Braje, Wilfried Lubisch, Gerd Steiner
  • Publication number: 20100137282
    Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.
    Type: Application
    Filed: April 16, 2008
    Publication date: June 3, 2010
    Inventors: David Evan Davies, David Thomas Davies, Ilaria Giordano, Alan Joseph Hennessy, Neil David Pearson
  • Publication number: 20100130470
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Application
    Filed: July 19, 2007
    Publication date: May 27, 2010
    Inventors: Heinz W. Pauls, Jailall Ramnauth, Peter Sampson, Andras Toro
  • Patent number: 7718646
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: May 18, 2010
    Assignee: Sanofi-Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Patent number: 7622460
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: November 24, 2009
    Assignee: sanofi-aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20090239839
    Abstract: An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.
    Type: Application
    Filed: February 24, 2009
    Publication date: September 24, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Fumio ITOH, Shuji Hinuma, Naoyuki Kanzaki, Hiroshi Mabuchi, Hiromi Yoshida, Hirokazu Matsumoto, Takeshi Wakabayashi
  • Publication number: 20090156578
    Abstract: In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.
    Type: Application
    Filed: December 1, 2006
    Publication date: June 18, 2009
    Inventors: Henry Pauls, Judd M. Berman
  • Publication number: 20090093457
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 10, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20090042858
    Abstract: The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.
    Type: Application
    Filed: June 16, 2006
    Publication date: February 12, 2009
    Inventors: Paul Barsanti, Nathan Brammier, Bryan Chang, Zhi-Jie Ni, Weibo Wang, Amy Weiner
  • Publication number: 20080261949
    Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen a
    Type: Application
    Filed: June 24, 2008
    Publication date: October 23, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
  • Publication number: 20080227770
    Abstract: A compound represented by the formula [1]: wherein ring A and ring B each represent an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl group optionally substituted with an optionally substituted hydroxyl group; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; x2 represents a bond, —O— or —S—; X3 represents a bond or an optionally substituted divalent hydrocarbon group; Y represents an optionally esterified or amidated carboxyl group, or a salt thereof. The compound of the formula [I] is safer and has more potent lipid lowering activity such as squalene synthase inhibitory activity (cholesterol lowering activity) and triglyceride lowering activity, and thus it is a compound useful as an agent for preventing or treating hyperlipemia.
    Type: Application
    Filed: July 30, 2004
    Publication date: September 18, 2008
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shogo Marui, Takashi Miki, Shoutarou Miura, Tomoyuki Nishimoto, Yoshihisa Nakada
  • Patent number: 7425550
    Abstract: A compound of formula I is provided having the structure wherein W is as defined herein; X is —CHR5O—; Y is a bond; Z is an aryl or heteroaryl group; and R1, and R2, are as described herein. Further provided is a method for treating diabetes and related diseases employing the above compound, either alone or in combination with another therapeutic agent.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 16, 2008
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Philip Sher, Gang Wu, Terry Stouch, Bruce Ellsworth
  • Patent number: 7390798
    Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.
    Type: Grant
    Filed: February 9, 2005
    Date of Patent: June 24, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
  • Patent number: 7354914
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Grant
    Filed: November 29, 2004
    Date of Patent: April 8, 2008
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Publication number: 20080031817
    Abstract: Though copper is elevated in the tumor tissue and plasma of patients with various malignancies, the molecular targets for copper binding agents in angiogenesis and tumor progression remain poorly understood. It is disclosed that one anti-angiogenic target for the copper binding agent tetrathiomolybdate is intracellular CuZn-superoxide dismutase (SOD1). A second generation tetrathiomolybdate analog, ATN-224, inhibits endothelial cell (EC) proliferation in vitro, binds to SOD1 and inhibits its activity without displacing bound copper ATN-224 can accumulate in ECs and inhibit CuZnSOD activity with an IC50 similar to the IC50 for EC proliferation, resulting in increased generation of intracellular reactive oxygen species. Inhibition of EC proliferation by ATN-224 in vitro is substantially reversed by a synthetic porphyrin SOD mimetic. Similar results were observed in vivo, where inhibition of angiogenesis by ATN-224 in a Matrigel plug model was also reversed by MnTBAP.
    Type: Application
    Filed: February 24, 2005
    Publication date: February 7, 2008
    Inventors: Andrew P. Mazar, Steven Pirie-Shepherd, Oscar Betancourt
  • Patent number: 7294622
    Abstract: Compounds having the formula (I) pharmaceutical compositions containing them and their methods of use for the treatment of neurological disorders related to amyloid ? protein production and neurological disorders such as Alzheimer's disease. These compounds inhibit ? secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein.
    Type: Grant
    Filed: October 2, 2003
    Date of Patent: November 13, 2007
    Assignee: Astrazeneca AB
    Inventors: Christopher Becker, Bruce Dembofsky, Robert Jacobs, James Kang, Cyrus Ohnmacht, James Rosamond, Ashokkumar Bhikkappa Shenvi, Thomas Simpson, James Woods
  • Patent number: 7288559
    Abstract: The present invention is directed to compounds that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: March 10, 2004
    Date of Patent: October 30, 2007
    Assignee: Merck + Co, Inc.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, C. Blair Zartman
  • Patent number: 7232813
    Abstract: The invention relates to a novel use of known benzazepine, benzoxazepine, benzo-thiazepine-N-acetic acid and phosphono-substituted benzazepinone derivatives having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity. The compounds of the invention are useful for the preparation of pharmaceutical compositions for prophylaxis and treatment of neurodegenerative disorders. The compounds of the invention are known from the European patents EP 0 733 642 and EP 0 916 679, and can be described by the general formulae (1): wherein the symbols have the meanings as given above in the description.
    Type: Grant
    Filed: January 7, 2005
    Date of Patent: June 19, 2007
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Hrissanthi Ikonomidou, Lechoslaw A. Turski, Dieter Ziegler, Michael Weske
  • Patent number: 7211573
    Abstract: The invention relates to compounds of the formula I wherein R, R1, R2, R3, X, and n are defined in the specification. The invention also provides pharmaceutically suitable acid addition salts thereof and all forms of optically pure enantiomers, recemates or diastereomers and diastereomeric mixtures thereof. Compounds of the invention are useful for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: May 1, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 6977252
    Abstract: The present invention relates to use of compounds represented by the following general formula [1] or salts or prodrugs thereof: [where R1 represents hydrogen atom or lower alkoxy group; R2 represents hydrogen atom, lower alkoxy group, optionally substituted phenyl group, (where R3 represents acyl group); X represents —CO— or —CH2—; and n-represents 1 or 2], as drugs for overcoming a resistance to anticancer drugs or drugs for enhancing an effect of anticancer drugs. The compounds represented by the general formula [1] have not only a function of overcoming the resistance to various anticancer drugs but also a function of enhancing the effect of various anticancer drugs to anticancer-drug sensitive cells. Thus, these compounds have excellent effects on resistant cells and also on sensitive cells, and in particular effective in the treatment of a cancer having an acquired resistance to an anticancer drug.
    Type: Grant
    Filed: May 19, 2000
    Date of Patent: December 20, 2005
    Assignee: Noboru Kaneko
    Inventors: Noboru Kaneko, Kazuhito Nishio, Takashi Nakamura
  • Patent number: 6924277
    Abstract: Compounds having the general formula wherein R1a, R1b, R1c, X1, X2, R2, R3, R4, R5, R6, n, Y and Z are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.
    Type: Grant
    Filed: September 27, 2001
    Date of Patent: August 2, 2005
    Assignee: AstraZeneca AB
    Inventor: Peter Bernstein
  • Patent number: 6906056
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Grant
    Filed: March 20, 2003
    Date of Patent: June 14, 2005
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: Richard C. Thompson, Stephen Wilkie, Douglas R. Stack, Eldon E. Vanmeter, Qing Shi, Thomas C. Britton, James E. Audia, Jon K. Reel, Thomas E. Mabry, Bruce A. Dressman, Cynthia L. Cwi, Steven S. Henry, Stacey L. McDaniel, Russell D. Stucky, Warren J. Porter
  • Patent number: 6897305
    Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel , thereby modulating the biological activities thereof.
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: May 24, 2005
    Assignee: Theravance, Inc.
    Inventors: Yu-Hua Ji, Maya Natarajan, John H. Griffin, Thomas E. Jenkins
  • Publication number: 20040192669
    Abstract: Phenolic compounds with a phenolic molecule to which are covalently linked an oxygen-containing group, a nitrogen or another oxygen containing group, and a C1-C4 alkoxy group, obtainable from monocotyledonous plants, or by chemical synthesis, have been found to act as weight loss agents, appetite suppressants, mood enhancers and adjunctive therapy for arthritis, sleep apnea, fibromyalgia, diabetes and hyperglycemia. Additional chemical compounds of the present invention may include benzoxazinoids-cyclic hydroxyamic acids, lactams, and corresponding glucosides, which may serve as precursors to phenolic compounds. The phenolic compounds and precursors of phenolic compounds of the present invention, at concentrations suitable for human therapeutic use, may be obtained from monocotyledonous plants such as corn in their early growth states which are timely harvested for optimum yield.
    Type: Application
    Filed: November 20, 2003
    Publication date: September 30, 2004
    Inventors: Mark J. Rosenfeld, Scott R. Forsberg